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学科主题: 氟化学 ; 生命有机化学
题名: Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses
其他题名: Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses
作者: LE GIANG ; VANDEGRAAFF NICK ; RHODES DAVID I ; JONES ERIC D ; COATES JONATHAN A V ; Lv L(吕龙) ; LI XINMING ; YU CHANGJIANG ; FENG XIAO ; DEADMAN JOHN J
通讯作者: LE GIANG ; DEADMAN JOHN J
刊名: Bioorg. Med. Chem. Lett.
发表日期: 2010
卷: 20, 期:17, 页:5013-5018
收录类别: SCI
部门归属: Avexa公司; 中国科学院上海有机化学研究所
英文摘要: A series of novel HIV integrase inhibitors active against rategravir resistant strains are reported. Initial SAR studies revealed that activities against wild-type virus were successfully maintained at single digit nanomolar level with a wide range of substitutions. However, inclusion of nitrogen-based cyclic substitutions was crucial for achieving potency against mutant viruses. Several compounds with excellent activities against wild-type virus as well as against the viruses with the mutations Q148H/G140S or N155H/E92Q were reported. (C) 2010 Elsevier Ltd. All rights reserved.
语种: 英语
相关网址: 查看原文
WOS记录号: WOS:000281247000007
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内容类型: 期刊论文
URI标识: http://ir.sioc.ac.cn/handle/331003/19233
Appears in Collections:中科院有机氟化学重点实验室_期刊论文

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Recommended Citation:
LE GIANG,VANDEGRAAFF NICK,RHODES DAVID I,et al. Discovery of potent HIV integrase inhibitors active against raltegravir resistant viruses[J]. Bioorg. Med. Chem. Lett.,2010,20(17):5013-5018.
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